DR 2313

Modify Date: 2024-01-09 16:49:49

DR 2313 Structure
DR 2313 structure
Common Name DR 2313
CAS Number 284028-90-6 Molecular Weight 182.243
Density 1.5±0.1 g/cm3 Boiling Point 349.3±52.0 °C at 760 mmHg
Molecular Formula C8H10N2OS Melting Point N/A
MSDS USA Flash Point 165.0±30.7 °C

 Use of DR 2313


DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo[1][2].

 Names

Name 7,8-Dihydro-2-methyl-1H-thiopyrano[4,3-d]pyrimidin-4(5H)-one
Synonym More Synonyms

 DR 2313 Biological Activity

Description DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo[1][2].
Related Catalog
Target

PARP-1:0.20 μM (IC50)

PARP-2:0.24 μM (IC50)

In Vitro DR2313 (0.016-16.4 μM; 30 min) inhibits poly(ADP-ribosyl)ation reaction in nuclear extracts of rat brain, with a Ki of 0.23 μM[1]. DR2313 shows more powerful inhibition of the poly(ADP-ribosyl)ation in the nuclear extracts of the rat brain (IC50=0.20 μM) than 3AB (35.4 μM), PND (0.56 μM), DIQ (2.96 μM), and DPQ (0.96 μM)[1]. DR2313 (1-100 μM; 10 min) shows a weak inhibition of the mono(ADP-ribosyl)ation in a concentration-dependent manner (IC50=59 μM)[1]. DR2313 (0.1-30 μM; pretreated for 30 min) reduces hydrogen peroxide (500 μM; 4 h) or glutamate (1 mM; 30 min) induced excessive formation of poly(ADP-ribose) and cell death[1].
In Vivo DR2313 (3-10 mg/kg i.v. bolus or infusion for 6 h) significantly reduces the cortical infarct volume in both permanent and transient focal ischemia models in rats[1]. Animal Model: Male Wistar rats (220-300 g) with permanent MCA occlusions (pMCAos) and transient MCA occlusions (tMCAos)[1] Dosage: 3, 10 mg/kg Administration: I.v. bolus and i.v. infusion for 6 h beginning 5 min before the onset of ischemia Result: Reduced the infarct volume in a dose-dependent manner in pMCAo and tMCAo model.
References

[1]. Nakajima H, et, al. A newly synthesized poly(ADP-ribose) polymerase inhibitor, DR2313 [2-methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]: pharmacological profiles, neuroprotective effects, and therapeutic time window in cerebral ischemia in rats. J Pharmacol Exp Ther. 2005 Feb;312(2):472-81.

[2]. Xu Z, et, al. Endonuclease G does not play an obligatory role in poly(ADP-ribose) polymerase-dependent cell death after transient focal cerebral ischemia. Am J Physiol Regul Integr Comp Physiol. 2010 Jul;299(1):R215-21.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 349.3±52.0 °C at 760 mmHg
Molecular Formula C8H10N2OS
Molecular Weight 182.243
Flash Point 165.0±30.7 °C
Exact Mass 182.051376
PSA 71.05000
LogP 0.66
Vapour Pressure 0.0±0.8 mmHg at 25°C
Index of Refraction 1.714
Storage condition 2~8°C

 Safety Information

Hazard Codes Xn
RIDADR NONH for all modes of transport
HS Code 2934999090

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

2-Methyl-1,5,7,8-tetrahydro-4H-thiopyrano[4,3-d]pyrimidin-4-one
3,5,7,8-Tetrahydro-2-methyl-4H-thiopyrano[4,3-d]pyrimidin-4-one
2-methyl-3,5,7,8-tetrahydrothiopyrano(4,3-d)pyrimidine-4-one
7,8-Dihydro-2-methyl-1H-thiopyrano[4,3-d]pyrimidin-4(5H)-one
4H-Thiopyrano[4,3-d]pyrimidin-4-one, 1,5,7,8-tetrahydro-2-methyl-
DR 2313
1,5,7,8-TETRAHYDRO-2-METHYL-4H-THIOPYRANO[4,3-D]PYRIMIDIN-4-ONE
2-Methyl-1-sulfanyl-1H,4H,5H,7H,8H-pyrano[4,3-d]pyriMidin-4-one
3,5,7,8-tetrahydro-2-methyl-4h-thiopyrano(4,3-d)pyrimidin-4-one
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